Influence of pH on the inhibitory action of local anaesthetics on smooth muscle contraction. 1970

A Antonio, and M Rocha e Silva, and Y Yashuda

1. The guinea-pig isolated ileum kept in a calcium-free depolarizing solution contracts when calcium is added; the responses are proportional to the concentration of calcium and are reversed by washing.2. The contractions elicited by calcium are inhibited by three different classes of compounds: local anaesthetics, pentobarbitone and ethanol. The inhibitory action of the local anaesthetics increases with an increase in pH, the inhibitory action of pentobarbitone increases with a decrease in pH and the inhibitory action of ethanol is not affected by variations in Tyrode pH.3. It is suggested that the antagonists are active when unionized and that the inhibition is obtained when unionized compounds have dissolved in the lipid material of the cell membrane. The possible site of action of the antagonists is discussed.

UI MeSH Term Description Entries
D002118 Calcium A basic element found in nearly all tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes. Coagulation Factor IV,Factor IV,Blood Coagulation Factor IV,Calcium-40,Calcium 40,Factor IV, Coagulation
D002462 Cell Membrane The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells. Plasma Membrane,Cytoplasmic Membrane,Cell Membranes,Cytoplasmic Membranes,Membrane, Cell,Membrane, Cytoplasmic,Membrane, Plasma,Membranes, Cell,Membranes, Cytoplasmic,Membranes, Plasma,Plasma Membranes
D003042 Cocaine An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. Cocaine HCl,Cocaine Hydrochloride,HCl, Cocaine,Hydrochloride, Cocaine
D000431 Ethanol A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in ALCOHOLIC BEVERAGES. Alcohol, Ethyl,Absolute Alcohol,Grain Alcohol,Alcohol, Absolute,Alcohol, Grain,Ethyl Alcohol
D000779 Anesthetics, Local Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. Anesthetics, Conduction-Blocking,Conduction-Blocking Anesthetics,Local Anesthetic,Anesthetics, Topical,Anesthetic, Local,Anesthetics, Conduction Blocking,Conduction Blocking Anesthetics,Local Anesthetics,Topical Anesthetics
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

Related Publications

A Antonio, and M Rocha e Silva, and Y Yashuda
September 1968, Life sciences,
A Antonio, and M Rocha e Silva, and Y Yashuda
January 1976, Pharmacology,
A Antonio, and M Rocha e Silva, and Y Yashuda
January 1948, Quarterly journal of pharmacy and pharmacology,
A Antonio, and M Rocha e Silva, and Y Yashuda
September 1948, The Pharmaceutical journal,
A Antonio, and M Rocha e Silva, and Y Yashuda
January 1987, Acta cientifica venezolana,
A Antonio, and M Rocha e Silva, and Y Yashuda
May 1978, Prostaglandins,
A Antonio, and M Rocha e Silva, and Y Yashuda
April 1997, European journal of pharmacology,
A Antonio, and M Rocha e Silva, and Y Yashuda
January 1986, Drugs under experimental and clinical research,
A Antonio, and M Rocha e Silva, and Y Yashuda
September 1992, Nihon rinsho. Japanese journal of clinical medicine,
A Antonio, and M Rocha e Silva, and Y Yashuda
May 2012, The Journal of pharmacy and pharmacology,
Copied contents to your clipboard!